This invention relates to certain octahydro-6-azaindole dipeptide derivatives and pharmaceutical compositions thereof which have inhibitory activity against angiotensin converting enzyme and are therefore useful in the treatment of certain cardiovascular disorders including hypertension and heart failure.
The enzyme renin is produced in the kidney, it acts upon an alpha-2-globulin to release a decapeptide angiotensin I. Angiotensin converting enzyme cleaves a terminal dipeptide unit from angiotensin I to produce an octapeptide, angiotensin II, which is a highly potent pressor substance. In addition to a direct pressor effect, angiotensin II stimulates the release of aldosterone which also tends to elevate blood pressure by causing retention of sodium chloride and water. Abnormal activation of the renin-angiotensin hormonal control system is thought to be an important contributory factor in certain types of hypertensive disease and cogestive heart failure and inhibition of angiotensin converting enzyme is now well established as an effective approach in the treatment of these conditions.